Discovery of an SSTR2-Targeting Maytansinoid Conjugate (PEN-221) with Potent Activity in Vitro and in Vivo

Somatostatin receptor 2 (SSTR2) is frequently overexpressed on several types of solid tumors, including neuroendocrine tumors and small-cell lung cancer. Peptide agonists of SSTR2 are rapidly internalized upon binding to the receptor and linking a toxic payload to an SSTR2 agonist is a potential met...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 62; no. 5; pp. 2708 - 2719
Main Authors:	White, Brian H, Whalen, Kerry, Kriksciukaite, Kristina, Alargova, Rossitza, Au Yeung, Tsun, Bazinet, Patrick, Brockman, Adam, DuPont, Michelle, Oller, Haley, Lemelin, Charles-Andre, Lim Soo, Patrick, Moreau, Benoît, Perino, Samantha, Quinn, James M, Sharma, Gitanjali, Shinde, Rajesh, Sweryda-Krawiec, Beata, Wooster, Richard, Bilodeau, Mark T
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 14-03-2019
Subjects:	Animals Antineoplastic Agents, Phytogenic - chemistry Antineoplastic Agents, Phytogenic - pharmacokinetics Antineoplastic Agents, Phytogenic - pharmacology Cell Line CHO Cells Cricetulus Dogs Drug Discovery Humans Immunoconjugates - chemistry Immunoconjugates - pharmacology Maytansine - chemistry Maytansine - pharmacokinetics Maytansine - pharmacology Mice Receptors, Somatostatin - drug effects Receptors, Somatostatin - metabolism Xenograft Model Antitumor Assays
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